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Literature DB >> 24900658

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

Jin-Jun Liu¹, Brian Higgins¹, Grace Ju¹, Kenneth Kolinsky¹, Kin-Chun Luk¹, Kathryn Packman¹, Giacomo Pizzolato¹, Yi Ren¹, Kshitij Thakkar¹, Christian Tovar¹, Zhuming Zhang¹, Peter M Wovkulich¹.

Abstract

A new series of 7,8-disubstituted pyrazolobenzodiazepines based on the lead compound 1 have been synthesized and evaluated for their effects on mitosis and angiogenesis. Described herein is the design, synthesis, SAR, and antitumor activity of these compounds leading to the identification of R1530, which was selected for clinical evaluation.

Entities: Chemical Disease Gene

Keywords: FGFr and PDGFr-β; VGFr-2; antitumor effect; mitosis/angiogenesis inhibitor; pyrazolobenzodiazepines

Year: 2013 PMID： 24900658 PMCID： PMC4027509 DOI： 10.1021/ml300351e

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

18 in total

Review 1. Mechanisms of angiogenesis.

Authors: W Risau
Journal: Nature Date: 1997-04-17 Impact factor: 49.962

Review 2. The benzodiazepine story.

Authors: L H Sternbach
Journal: Prog Drug Res Date: 1978

3. Anti-angiogenesis: new concept for therapy of solid tumors.

Authors: J Folkman
Journal: Ann Surg Date: 1972-03 Impact factor: 12.969

4. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.

Authors: Christian Tovar; Brian Higgins; Dayanand Deo; Kenneth Kolinsky; Jin-Jun Liu; David C Heimbrook; Lyubomir T Vassilev
Journal: Cell Cycle Date: 2010-08-21 Impact factor: 4.534

5. Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

Authors: Jin-Jun Liu; Irena Daniewski; Qingjie Ding; Brian Higgins; Grace Ju; Kenneth Kolinsky; Fred Konzelmann; Christine Lukacs; Giacomo Pizzolato; Pamela Rossman; Amy Swain; Kshitij Thakkar; Chung-Chen Wei; Dorota Miklowski; Hong Yang; Xuefeng Yin; Peter M Wovkulich
Journal: Bioorg Med Chem Lett Date: 2010-08-21 Impact factor: 2.823

6. Preclinical evaluation of tumor microvascular response to a novel antiangiogenic/antitumor agent RO0281501 by dynamic contrast-enhanced MRI at 1.5 T.

Authors: Manickam Muruganandham; Mihaela Lupu; Jonathan P Dyke; Cornelia Matei; Michael Linn; Kathryn Packman; Kenneth Kolinsky; Brian Higgins; Jason A Koutcher
Journal: Mol Cancer Ther Date: 2006-08 Impact factor: 6.261

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

Review 1. Mechanisms of angiogenesis.

Review 2. The benzodiazepine story.

3. Anti-angiogenesis: new concept for therapy of solid tumors.

4. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.

5. Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

6. Preclinical evaluation of tumor microvascular response to a novel antiangiogenic/antitumor agent RO0281501 by dynamic contrast-enhanced MRI at 1.5 T.

Review 7. Combination of antiangiogenesis with chemotherapy for more effective cancer treatment.

Review 8. The future of tyrosine kinase inhibitors: single agent or combination?

Review 9. Combination targeted therapy in advanced renal cell carcinoma.

Review 10. Angiogenesis: an organizing principle for drug discovery?

Review 1. Pyrazoles as potential anti-angiogenesis agents: a contemporary overview.